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HRP20141065T1 - Derivati difenil-sulfida i lijekovi koji ih sadrže kao aktivni sastojak - Google Patents

Derivati difenil-sulfida i lijekovi koji ih sadrže kao aktivni sastojak Download PDF

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HRP20141065T1
HRP20141065T1 HRP20141065AT HRP20141065T HRP20141065T1 HR P20141065 T1 HRP20141065 T1 HR P20141065T1 HR P20141065A T HRP20141065A T HR P20141065AT HR P20141065 T HRP20141065 T HR P20141065T HR P20141065 T1 HRP20141065 T1 HR P20141065T1
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amino
group
acid monoester
carbon atoms
chloro
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Yasushi Kohno
Kiyoshi Fujii
Momoko Taru
Keita Miyoshi
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Kyorin Pharmaceutical Co., Ltd.
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Claims (12)

1. Derivat difenil-sulfida, ili njegova farmaceutski prihvatljiva sol ili hidrat, prikazan općom formulom (1), [image] , naznačen time što u formuli (1) R1 predstavlja atom vodika, atom halogena, trifluormetilnu skupinu, izborno supstituiranu alkilnu skupinu s 1 do 6 atoma ugljika, izborno supstituiranu cikloalkilnu skupinu s 3 do 6 atoma ugljika, izborno supstituiranu arilnu skupinu s 6 do 10 atomu ugljiku, izborno supstituiranu alkoksi skupinu s 1 do 4 atoma ugljika, izborno supstituiranu benziloksi skupinu, izborno supstituiranu acilnu skupinu s 1 do 4 atoma ugljika, cijano skupinu ili karboksilnu skupinu; R2 predstavlja izborno supstituiranu alkilnu skupinu s 1 do 6 atoma ugljika ili izborno supstituiranu alkenilnu skupinu s 2 do 6 atoma ugljika; X predstavlja metilensku skupinu, koja može biti supstituirana s 1 ili 2 atoma fluora ili predstavlja atom kisika; Y predstavlja atom vodika ili izborno supstituiranu alkilnu skupinu s 1 do 6 atoma ugljika; i Z predstavlja atom halogena; te što se svakog od izbornih supstituenata "alkilne skupine s 1 do 6 atoma ugljika", "cikloalkilne skupina s 3 do 6 atoma ugljika, "arilne skupine s 6 do 10 atoma ugljika, "alkoksi skupine s 1 do 4 atoma ugljika", "benziloksi skupine", "acilne skupine s 1 do 4 atoma ugljika" i "alkenilne skupine s 2 do 6 atoma ugljika" neovisno bira iz skupine koju čine atom halogena, trifluormetilna skupina, alkilna skupina s 1 do 6 atoma ugljika, cikloalkilna skupina s 3 do 6 atoma ugljika, arilna skupina s 6 do 10 atoma ugljika, alkoksi skupina s 1 do 4 atoma ugljika, benziloksi skupina, acilna skupina s 1 do 4 atoma ugljika, cijano skupina, alkenilna skupina s 2 do 6 atoma ugljika, hidroksilna skupina, nitro skupina i amino skupina.
2. Derivat difenil-sulfida u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol ili hidrat, naznačen time što je spoj prikazan općom formulom (1) prikazan općom formulom (1a), [image] , gdje su u formuli (1a) R1, R2, X i Y definirani kao gore.
3. Derivat difenil-sulfida u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol ili hidrat, naznačen time što je spoj prikazan općom formulom (1) prikazan općom formulom (1b), [image] , gdje u formuli (1b) Xa predstavlja atom kisika ili -CH2-, a R1, R2 i Y su definirani kao gore.
4. Derivat difenil-sulfida u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol ili hidrat, naznačen time što je spoj prikazan općom formulom (1) prikazan općom formulom (1c), [image] , gdje su u formuli (1c) R1 i R2 definirani kao gore.
5. Derivat difenil-sulfida u skladu s patentnim zahtjevom 4, ili njegova farmaceutski prihvatljiva sol ili hidrat, naznačen time što R1 predstavlja trifluormetilnu skupinu, alkilnu skupinu s 1 do 6 atoma ugljika, cikloalkilnu skupinu s 3 do 6 atoma ugljika, arilnu skupinu s 6 do 10 atoma ugljika ili benziloksi skupinu.
6. Derivat difenil-sulfida u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol ili hidrat, naznačen time što spoj je prikazan općom formulom (1) monoester (S)-2-amino-4-[2-klor-4-(2-hidroksi-5-trifluormetilfeniltio)fenil]-2-propilbutilfosforne kiseline, monoester (R)-2-alil-2-amino-4-[2-klor-4-(2-hidroksi-5-trifluormetilfeniltio)fenil]butilfosforne kiseline, monoester (S)-2-amino-4-[2-klor-4-(2-hidroksi-5-trifluormetilfeniltio)fenil]-2-metilbutilfosforne kiseline, monoester (S)-2-amino-4-[2-klor-4-(2-hidroksi-5-izopropilfeniltio)fenil]-2-metilbutilfosforne kiseline, monoester (S)-2-amino-4-[2-klor-4-(5-ciklopropil-2-hidroksifeniltio)fenil)-2-metilbutilfosforne kiseline, monoester (S)-2-amino-4-[4-(5-benziloksi-2-hidroksifeniltio)-2-klorfenil]-2-metilbutilfosforne kiseline, monoester (S)-2-amino-4-[2-klor-4-(2-hidroksi-5-propilfeniltio)fenil]-2-propilbutilfosforne kiseline, monoester (S)-2-amino-4-[2-klor-4-(2-hidroksi-5-izopropilfeniltio)fenil]-2-propilbutilfosforne kiseline, monoester (S)-2-amino-4-[2-klor-4-(5-ciklopropil-2-hidroksifeniltio)fenil]-2-propilbutilfosforne kiseline, monoester (S)-2-amino-4-[4-(5-t-butil-2-hidroksifeniltio)-2-klorfenil]-2-propilbutilfosforne kiseline, monoester (S)-2-amino-4-[2-klor-4-(2-hidroksi-5-bifeniltio)fenil]-2-propilbutilfosforne kiseline, ili monoester (S)-2-amino-4-[4-(5-benziloksi-2-hidroksifeniltio)-2-klorfenil]-2-propilbutilfosforne kiseline.
7. Derivat difenil-sulfida u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol ili hidrat, naznačen time što je spoj prikazan općom formulom (1) monoester (–)-2-amino-4-[2-klor-4-(2-hidroksi-5-trifluormetilfeniltio)fenil]-2-propilbutilfosforne kiseline, monoester (–)-2-alil-2-amino-4-[2-klor-4-(2-hidroksi-5-trifluormetilfeniltio)fenil]butilfosforne kiseline, monoester (–)-2-amino-4-[2-klor-4-(2-hidroksi-5-trifluormetilfeniltio)fenil]-2-metilbutilfosforne kiseline, monoester (–)-2-amino-4-[2-klor-4-(2-hidroksi-5-izopropilfeniltio)fenil]-2-metilbutilfosforne kiseline, monoester (–)-2-amino-4-[2-klor-4-(5-ciklopropil-2-hidroksifeniltio)fenil]-2-metilbutilfosforne kiseline, monoester (–)-2-amino-4-[4-(5-benziloksi-2-hidroksifeniltio)-2-klorfenil]-2-metilbutilfosforne kiseline, monoester (–)-2-amino-4-[2-klor-4-(2-hidroksi-5-propilfeniltio)fenil]-2-propilbutilfosforne kiseline, monoester (–)-2-amino-4-[2-klor-4-(2-hidroksi-5-izopropilfeniltio)fenil]-2-propilbutilfosforne kiseline, monoester (–)-2-amino-4-[2-klor-4-(5-ciklopropil-2-hidroksifeniltio)fenil]-2-propilbutilfosforne kiseline, monoester (–)-2-amino-4-[4-(5-t-butil-2-hidroksifeniltio)-2-klorfenil]-2-propilbutilfosforne kiseline, monoester (–)-2-amino-4-[2-klor-4-(2-hidroksi-5-bifeniltio)fenil]-2-propilbutilfosforne kiseline, ili monoester (–)-2-amino-4-[4-(5-benziloksi-2-hidroksifeniltio)-2-klorfenil]-2-propilbutilfosforne kiseline.
8. Lijek koji se bazira na antagonističkom djelovanju na receptor za sfingozin-1-fosfat 3 (S1P3), naznačen time što lijek kao aktivni sastojak sadrži derivat difenil-sulfida u skladu s bilo kojim od patentnih zahtjeva 1 do 7, ili njegovu farmaceutski prihvatljivu sol ili hidrat.
9. Lijek u skladu s patentnim zahtjevom 8, naznačen time što lijek je lijek namijenjen terapiji ili sprječavanju kontrakcije dišnog sustava, bronhijalne astme, kronične opstruktivna plućne bolesti (COPD), plućnog emfizema, trahealne stenoze, difuznog panbronhiolitisa, bronhitisa kao posljedice infekcije, bolesti vezivnog tkiva, ili kod presađivanja, difuzne plućne hamartoangiomiomatoze, sindroma respiratornog distresa kod odraslih (ARDS), intersticijskog pneumonitisa, raka pluća, pneumonične preosjetljivisti, idiopatske intersticijske pneumonije, fibroze pluća, sepse, ili citokinske oluje uzrokovane infekcijom virusom influence ili virusom RS.
10. Lijek u skladu s patentnim zahtjevom 8, naznačen time što lijek je lijek namijenjen terapiji arterijske skleroze, hipertrofija intime krvnih žila, čvrstih tumora, dijabetičke retinopatije, reumatoidnog artritisa, zastoja rada srca, ishemijsko-reperfuzijskih poremećaja, spazama cerebralnih krvna žila nakon subarahnoidalnog krvarenja, angine pektoris ili infarkta miokarda uzrokovanog spazmima koronarnih krvnih žila, glomerulonefritisa, tromboze, bolesti pluća uzrokovane plućnim edemom, srčane aritmije, očne bolesti, očne hipertenzije, glaukoma, glaukomatozne retinopatije, optičke neuropatije ili degeneracije žute pjege.
11. Lijek u skladu s patentnim zahtjevom 8, naznačen time što lijek je lijek namijenjen terapiji ili sprječavanju sepse.
12. Farmaceutski pripravak, naznačen time što sadrži derivat difenil-sulfida u skladu s bilo kojim od patentnih zahtjeva 1 do 7, ili njegovu farmaceutski prihvatljivu sol ili hidrat, kao i farmaceutski prihvatljivu podlogu.
HRP20141065AT 2009-07-09 2010-07-08 Derivati difenil-sulfida i lijekovi koji ih sadrže kao aktivni sastojak HRP20141065T1 (hr)

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JP2009162289 2009-07-09
JP2010112138 2010-05-14
EP10796915.6A EP2452944B1 (en) 2009-07-09 2010-07-08 Diphenyl sulfide derivatives and medicines containing them as active ingredient
PCT/JP2010/004453 WO2011004604A1 (ja) 2009-07-09 2010-07-08 ジフェニルスルフィド誘導体及びそれらを有効成分とする医薬

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BR112012000320A2 (pt) 2016-03-22
US8569270B2 (en) 2013-10-29
CN102471355A (zh) 2012-05-23
EP2452944B1 (en) 2014-09-10
ES2514665T3 (es) 2014-10-28
KR20120089234A (ko) 2012-08-09
WO2011004604A1 (ja) 2011-01-13
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EP2452944A1 (en) 2012-05-16
ZA201108459B (en) 2012-07-25
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CA2764126A1 (en) 2011-01-13
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